Areca, a type of palm tree also known as Areca catechu, is generally cultivated in India, Southeast Asia, the East Indies, Taiwan and East Africa. The fruit of the Areca tree is a nut containing a single seed having a thin seed coat. The nut of Areca catechu tree contains several pyridine-derived alkaloids, including arecoline, arecaidine, guvacoline, and guvacine which may be as high as 1.7% of the nut's makeup. In nature, the highest single alkaloid component concentration in Areca nut is arecoline, which contains a methyl ester functional group.
The Areca nut is known around the world for its stimulating effects as well as improved cognition and memory, and it is chewed by almost one-half billion people who seek these properties of the nut. Betel quid is the combination of Areca catechu nut and Piper betel leaf, and other lesser components, and is the most common use of the Areca plant. Betel quid chewing, however, has been shown to be a major etiologic factor in oral cancer among such users. It has been found that Areca nut tannins and arecoline inhibit the growth of oral mucosal fibroblasts and keratinocytes. The effects of long-term use include oral submucosal fibrosis, leukoplasia and oral cancer. Studies have shown that conventional Areca nut extracts induce DNA breaks and unscheduled DNA synthesis and differentiation of oral keratinocytes. Arecoline also displays genotoxic effects.
The autonomic effects of Areca nut on the user when chewing betel quid, include sweating and facial flush, and increases in skin temperature and heart rate. Specifically, the alkaloids arecoline and arecaidine, although initially causing a brief depressor response, subsequently produce an increase in arterial blood pressure and heart rate. These stimuli are mediated through muscarinic M1 receptors. In animals, arecoline, Arecaidine, guvacoline, and guvacine are known to possess activity as agonists at muscarinic acetylcholine receptors. Additionally, arecoline has been shown to have indirect effects on catecholamine levels, while arecaidine and guvacine inhibit gamma-aminobutyric acid (GABA) receptor uptake in micromolar concentrations.
Other botanical constituents having stimulating effects are found in the holly family, Aquifoliaceae. The genus Ilex is one such member and is found worldwide in subtropical and tropical regions of both hemispheres. I. paraguariensis, a perennial tree, is native to South America and is also known as maté or yerba maté. It is the most commercialized plant of South America. I. paraquariensis is used to prepare a tea-like maté beverage. The maté beverage is made from the dried, toasted and milled leaves and stems of the plant genus and widely consumed in Argentina, Paraguay, Uruguay, Southern Brazil, and more recently in North America, Europe, and the Middle East.
The maté beverage is consumed primarily as an infusion, either by the addition of boiling water to the dry plant material, or by repeated additions of almost boiling water to the plant material. This infusion allows for extraction of water soluble plant constituents. Exposure of persons who drink the maté beverage to such extracted compounds is significant when the numbers of people and amount of maté beverage consumed is considered. A large number of people regularly consume some amount of maté beverage. In South America, approximately 30% of the population drink more than one liter per day of maté beverage, and many persons use the beverage as treatment of various conditions such a mental and physical fatigue, headaches, obesity, nervous depression, rheumatic pains, and improved cognition. The estimates for caffeine intake due to maté beverage consumption exceed the caffeine intakes known for other beverages such as coffee.
Consequently, one outcome of consumption of maté beverage and conventional nutraceutical extractions, is the presence of caffeine-related disorders such as gastrointestinal problems, caffeine toxicity, jitteriness, generalized anxiety, and insomnia. The consumption of caffeine exaggerates stress and stress-related hormone release. Blood pressure is elevated and the risks for heart attack and stroke are increased when caffeine is routinely consumed. Because maté beverage is such a part of the social structure and cultural habits of so many people and the fact that it is being increasingly used as a nutraceutical medicinal agent, reducing the amount of maté consumed does not appear to be a viable method for reducing caffeine consumption. An additional problem is that the maté that is consumed is made from raw maté plant material, which has varying amounts of caffeine when consumed drink to drink or dose to dose. This variability can cause confusing symptoms in users, hence, making the diagnosis of physiological problems difficult. In addition, such variability can cause uneven results when maté is used for treatment of various physiological conditions. A final issue regarding maté is that clinical and epidemiologic studies have found a positive association between maté consumption and cancer of the esophagus, oral cavity, pharynx, larynx, stomach and bladder.
Theobromine is best known for its effects in chocolate products. Theobromine has been synthesized and has been used as a drug to treat different medical conditions. For example, theobromine has been used as a diuretic making it particularly useful after a person has experienced cardiac failure. Cardiac failure often results in an excess accumulation of bodily fluids. Theobromine is also known for its ability to dilate blood vessels making it a commonly prescribed treatment for people suffering from high blood pressure. In addition, theobromine is known as a weak stimulant but does cause the jitteriness and hyper-anxiety associated with caffeine. As a stimulant, it has been noted to raise levels of serotonin making it an inexpensive anti-depressant. Theobromine also is an appetite suppressant and a useful adjunct for weight reduction. Theobromine remains in the body for a very long period of time. The half life after ingestion is approximately 6 hours. Another rather unique property of theobromine is its ability to relax bronchi in the lungs, which also has been used to treat asthmatic and pulmonary diseases. Theobromine has also been found to be relatively harmless in humans unless taken in excessive quantities.
What is needed then are compositions of combinations of extracts of Areca nut and extracts of maté, or extracts of Areca nut and theobromine, that provide desired physiological effects of improved memory, cognition and a sense of well being, appetite suppression, and have lowered amounts of carcinogens, such as arecoline and tannins. Such compositions would have medicinal value in improving mental focus and cognition, enhancing a sense of well being, reducing physical and mental fatigue and in treating obesity.